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The cannabinoid receptor 2 (CB2), is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the CNR2 gene. [5] [6] It is closely related to the cannabinoid receptor 1 (CB1), which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol (THC), the active agent in ...
Cannabinoid receptor 1 (CB1), is a G protein-coupled cannabinoid receptor that in humans is encoded by the CNR1 gene. [5] And discovered, by determination and characterization in 1988, [6] and cloned in 1990 for the first time. [7] [8] [9] The human CB1 receptor is expressed in the peripheral nervous system and central nervous system. [5]
A neurotransmitter for a possible endocannabinoid system in the brain and peripheral nervous system, anandamide (from 'ananda', Sanskrit for 'bliss'), was first characterized in 1992, [18] [19] [20] followed by discovery of other fatty acid neurotransmitters that behave as endogenous cannabinoids having a low-to-high range of efficacy for ...
3D model of 2-Arachidonoylglycerol, an endocannaboid. The endocannabinoid system (ECS) is a biological system composed of endocannabinoids, which are neurotransmitters that bind to cannabinoid receptors, and cannabinoid receptor proteins that are expressed throughout the central nervous system (including the brain) and peripheral nervous system.
Anandamide binds to the central (CB 1) and, to a lesser extent, peripheral (CB 2) cannabinoid receptors, where it acts as a partial agonist. Anandamide is about as potent as THC at the CB 1 receptor. [76] Anandamide is found in nearly all tissues in a wide range of animals. [77]
The plant-biosynthesized cannabinoid cannabidiol also shows "either direct or indirect activation" of TRPV1 receptors. [ 69 ] [ 42 ] TRPV1 colocalizes with CB1 receptors and CB2 receptors in sensory and brain neurons respectively, and other plant-cannabinoids like CBN , CBG , CBC , THCV , and CBDV are also agonists of this ion channel .
GPR55 is activated by the plant cannabinoids Δ 9-THC [12] and the endocannabinoids anandamide, 2-AG and noladin ether in the low nanomolar range. Exocannabinoids such as the synthetic cannabinoid CP-55940 are also able to activate the receptor [12] while the structurally unrelated cannabinoid mimic WIN 55,212-2 fails to activate the receptor. [10]
UR-144 (TMCP-018, KM-X1, MN-001, YX-17) is a drug invented by Abbott Laboratories, [2] that acts as a selective full agonist of the peripheral cannabinoid receptor CB 2, but with much lower affinity for the psychoactive CB 1 receptor.